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Publications in VIVO

Co-Author Network

Prossnitz, Eric Professor

Positions

Professor, Department of Internal Medicine 2015 -
Team Science Lead,, Clinical & Translational Science Center, Office of Research 2016 -
co-Director, Translational Cancer Biology and Signaling, UNM Cancer Center, University of New Mexico 2008 -

Postdoctoral Fellowship: The Scripps Research Institute

PhD: University of California at Berkeley

Research Interests
Estrogen is a critical factor in many diseases and cancers. Altering its activity through its multiple receptors is critical to the treatment of cancers and other diseases. We are developing new approaches to diagnose and treat breast, endometrial and ovarian cancers based on the discovery of a new estrogen receptor named GPR30/GPER. Our discovery of GPER-selective agonists and antagonists provide the opportunity to discover the roles of GPER in normal physiology and pathophysiology, including in metabolism (obesity and diabetes), cardiovascular function (atherosclerosis, hypertension), immune system (inflammation) and cancer.

Research Areas

selected publications

academic article
- Obligatory role for GPER in cardiovascular aging and disease. Science signaling. 9:-. 2016
- Towards a transcriptome-based theranostic platform for unfavorable breast cancer phenotypes. Proceedings of the National Academy of Sciences of the United States of America. :-. 2016
- GPER mediates the age-dependent upregulation of the myocardial endothelin system. Life sciences. :-. 2016
- GPER/GPR30 Knockout Mice: Effects of GPER on Metabolism. Methods in molecular biology (Clifton, N.J.). 1366:489-502. 2016
- Regulation of N-Formyl Peptide Receptor Signaling and Trafficking by Arrestin-Src Kinase Interaction. PloS one. 11:-. 2016
- G protein-coupled estrogen receptor inhibits vascular prostanoid production and activity. The Journal of endocrinology. :-. 2015
- Prostanoid-mediated contractions of the carotid artery become Nox2-independent with aging. Age (Dordrecht, Netherlands). 37:-. 2015
- International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacological reviews. 67:505-540. 2015
- What have we learned about GPER function in physiology and disease from knockout mice? The Journal of steroid biochemistry and molecular biology. :-. 2015
- Effects of Atrazine on Estrogen Receptor α- and G Protein-Coupled Receptor 30-Mediated Signaling and Proliferation in Cancer Cells and Cancer-Associated Fibroblasts. Environmental health perspectives. :-. 2015
- Estrogen-mediated inactivation of FOXO3a by the G protein-coupled estrogen receptor GPER. BMC cancer. 15:-. 2015
- Peptidyl arginine deiminase from Porphyromonas gingivalis abolishes anaphylatoxin C5a activity. The Journal of biological chemistry. 289:32481-32487. 2014
- Activation of GPER-1 estradiol receptor downregulates production of testosterone in isolated rat Leydig cells and adult human testis. 2014
- Endometrial cancer: molecular and cellular basis of tumor development, novel biomarkers and therapeutic agents, and innovative research approaches. Obstetrics and gynecology international. 2014:-. 2014
- Endothelin-1 but not angiotensin II contributes to functional aging in murine carotid arteries. Life sciences. :-. 2014
- Estrogen biology: new insights into GPER function and clinical opportunities. Molecular and cellular endocrinology. 389:71-83. 2014
- G Protein-coupled Estrogen Receptor Protects from Atherosclerosis. Scientific reports. 4:-. 2014
- G protein-coupled estrogen receptor (GPER) regulates mammary tumorigenesis and metastasis. Molecular cancer research : MCR. :-. 2014
- GPER mediates estrogen-induced signaling and proliferation in human breast epithelial cells and normal and malignant breast. Hormones & cancer. 5:146-160. 2014
- GPER-targeted, 99mTc-labeled, nonsteroidal ligands demonstrate selective tumor imaging and in vivo estrogen binding. Molecular cancer research : MCR. :-. 2014
- Introduction of D-phenylalanine enhanced the receptor binding affinities of gonadotropin-releasing hormone peptides. 2014
- Alike but not the same: anatomic heterogeneity of estrogen receptor-mediated vasodilation. Journal of cardiovascular pharmacology. 62:22-25. 2013
- Functional heterogeneity of NADPH oxidase-mediated contractions to endothelin with vascular aging. Life sciences. :-. 2013
- G protein-coupled estrogen receptor-selective ligands modulate endometrial tumor growth. Obstetrics and gynecology international. 2013:-. 2013
- GPER deficiency in male mice results in insulin resistance, dyslipidemia, and a proinflammatory state. Endocrinology. 154:4136-4145. 2013
- Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides. 2013
- Regulation of vascular smooth muscle tone by adipose-derived contracting factor. 2013
- The Concise Guide to PHARMACOLOGY 2013/14: overview. British journal of pharmacology. 170:1449-1458. 2013
- The G protein-coupled estrogen receptor (GPER) agonist G-1 expands the regulatory T-cell population under TH17-polarizing conditions. Journal of immunotherapy (Hagerstown, Md. : 1997). 36:190-196. 2013
- Deletion of G protein-coupled estrogen receptor increases endothelial vasoconstriction. Hypertension. 59:507-512. 2012
- G protein-coupled estrogen receptor: A new therapeutic target in stroke and traumatic brain/spinal cord injury?*. Critical care medicine. 40:3323-3325. 2012
- GPER regulates endothelin-dependent vascular tone and intracellular calcium. Life sciences. 91:623-627. 2012
- Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30. PloS one. 7:-. 2012
- Testosterone and secondary hypertension: new pieces to the puzzle. Hypertension. 59:1101-1103. 2012
- Activation of G protein-coupled estrogen receptor induces endothelium-independent relaxation of coronary artery smooth muscle. American journal of physiology. Endocrinology and metabolism. 301:E882-E888. 2011
- Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. The Journal of steroid biochemistry and molecular biology. 127:358-366. 2011
- Induction of interleukin-10 in the T helper type 17 effector population by the G protein coupled estrogen receptor (GPER) agonist G-1. Immunology. 134:93-106. 2011
- Mechanisms of estradiol-induced insulin secretion by the G protein-coupled estrogen receptor GPR30/GPER in pancreatic beta-cells. Endocrinology. 152:3030-3039. 2011
- Mesothelin and GPR30 staining among a spectrum of pancreatic epithelial neoplasms. International journal of surgical pathology. 19:588-596. 2011
- The G-protein-coupled estrogen receptor GPER in health and disease. Nature reviews. Endocrinology. 7:715-726. 2011
- GPR30 and estrogen receptor expression: new insights into hormone dependence of inflammatory breast cancer. Breast cancer research and treatment. 123:51-58. 2010
- Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs. Organic & biomolecular chemistry. 8:2252-2259. 2010
- Influence of charge on cell permeability and tumor imaging of GPR30-targeted 111in-labeled nonsteroidal imaging agents. ACS chemical biology. 5:681-690. 2010
- The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer research. 70:1184-1194. 2010
- Detection of intracellular granularity induction in prostate cancer cell lines by small molecules using the HyperCyt high-throughput flow cytometry system. Journal of biomolecular screening. 14:596-609. 2009
- Duplex high-throughput flow cytometry screen identifies two novel formylpeptide receptor family probes. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 75:253-263. 2009
- Expression of estrogen receptor GPR30 in the rat spinal cord and in autonomic and sensory ganglia. Journal of neuroscience research. 87:1610-1619. 2009
- GPR30 predicts poor survival for ovarian cancer. Gynecologic oncology. 114:465-471. 2009
- High-content screening: flow cytometry analysis. Methods in molecular biology (Clifton, N.J.). 486:151-165. 2009
- In vivo effects of a GPR30 antagonist. Nature chemical biology. 5:421-427. 2009
- Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity. Circulation research. 104:288-291. 2009
- A multifunctional androgen receptor screening assay using the high-throughput Hypercyt flow cytometry system. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 73:390-399. 2008
- Enhancement of somatostatin-receptor-targeted (177)Lu-[DOTA(0)-Tyr(3)]-octreotide therapy by gemcitabine pretreatment-mediated receptor uptake, up-regulation and cell cycle modulation. Nuclear medicine and biology. 35:673-678. 2008
- Estrogen signaling through the transmembrane G protein-coupled receptor GPR30. Annual review of physiology. 70:165-190. 2008
- GPR30: a novel therapeutic target in estrogen-related disease. Trends in pharmacological sciences. 29:116-123. 2008
- Preclinical development of a neutral, estrogen receptor-targeted, tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative for imaging of breast and endometrial cancers. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 49:978-986. 2008
- The ins and outs of GPR30: a transmembrane estrogen receptor. The Journal of steroid biochemistry and molecular biology. 109:350-353. 2008
- Activated N-formyl peptide receptor and high-affinity IgE receptor occupy common domains for signaling and internalization. Molecular biology of the cell. 18:1410-1420. 2007
- Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system. The Journal of endocrinology. 193:311-321. 2007
- G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells. Cancer research. 67:1859-1866. 2007
- Rapid-mix flow cytometry measurements of subsecond regulation of G protein-coupled receptor ternary complex dynamics by guanine nucleotides. Analytical biochemistry. 371:10-20. 2007
- Some mechanistic insights into GPCR activation from detergent-solubilized ternary complexes on beads. Advances in protein chemistry. 74:95-135. 2007
- Biomolecular screening of formylpeptide receptor ligands with a sensitive, quantitative, high-throughput flow cytometry platform. Nature protocols. 1:59-66. 2006
- Glutathione-S-transferase-green fluorescent protein fusion protein reveals slow dissociation from high site density beads and measures free GSH. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 69:326-334. 2006
- Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature chemical biology. 2:207-212. 2006
- High-throughput screening with HyperCyt flow cytometry to detect small molecule formylpeptide receptor ligands. Journal of biomolecular screening. 10:374-382. 2005
- Integration of virtual screening with high-throughput flow cytometry to identify novel small molecule formylpeptide receptor antagonists. Molecular pharmacology. 68:1301-1310. 2005
- Post-high-throughput screening analysis: an empirical compound prioritization scheme. Journal of biomolecular screening. 10:419-426. 2005
- Conformational regulation of alpha 4 beta 1-integrin affinity by reducing agents. "Inside-out" signaling is independent of and additive to reduction-regulated integrin activation. The Journal of biological chemistry. 279:32435-32443. 2004
- Flow cytometry for high-throughput, high-content screening. Current opinion in chemical biology. 8:392-398. 2004
- N-formyl peptide receptors cluster in an active raft-associated state prior to phosphorylation. The Journal of biological chemistry. 279:45175-45184. 2004
- FRET detection of cellular alpha4-integrin conformational activation. Biophysical journal. 85:3951-3962. 2003
- Ligand-receptor-G-protein molecular assemblies on beads for mechanistic studies and screening by flow cytometry. Molecular pharmacology. 64:1227-1238. 2003
- Synthesis and evaluation of novel gonadotropin-releasing hormone receptor-targeting peptides. Bioconjugate chemistry. 22:1682-1689.
- The G protein-coupled estrogen receptor GPER/GPR30 as a regulator of cardiovascular function.
review
- Emerging roles of GPER in diabetes and atherosclerosis. Trends in endocrinology and metabolism: TEM. 185-192. 2015

research overview

Research Interests
Estrogen is a critical factor in many cancers and altering its activity through its many receptors is critical to the treatment of cancers. We are developing new approaches to diagnose and treat breast, endometrial and ovarian cancers based on the discovery of a new estrogen receptor named GPR30.